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Tolterodine: Pediatric drug information

Tolterodine: Pediatric drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Tolterodine: Drug information" and "Tolterodine: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Detrol;
  • Detrol LA [DSC]
Brand Names: Canada
  • APO-Tolterodine [DSC];
  • Detrol;
  • Detrol LA;
  • JAMP-Tolterodine;
  • MINT-Tolterodine;
  • MYLAN-Tolterodine ER [DSC];
  • SANDOZ Tolterodine LA;
  • TEVA-Tolterodine;
  • TEVA-Tolterodine LA
Therapeutic Category
  • Anticholinergic Agent
Dosing: Adult

(For additional information see "Tolterodine: Drug information")

Dosage guidance:

Safety: Use with extreme caution or avoid use in patients with controlled (treated) narrow-angle glaucoma, history of urinary retention, bladder outlet obstruction, or decreased GI motility (Ref).

Overactive bladder

Overactive bladder, urinary urgency with or without incontinence (alternative agent): Note: Other therapies (eg, beta-3 adrenergic agonists) may be preferred in individuals who may be sensitive to anticholinergic effects (eg, dry mouth, constipation) (Ref) and in those with potential cognitive risks (Ref). Not used in stress type urinary incontinence (Ref).

Oral:

ER capsule (preferred): Note: May cause less dry mouth than the IR formulation (Ref).

Initial: 2 mg once daily (Ref).

Dosage adjustment: If needed, may increase to 4 mg once daily after 2 to 6 weeks based on response and tolerability (Ref).

IR tablet:

Initial: 1 mg twice daily (Ref).

Dosage adjustment: If needed, may increase to 2 mg twice daily after 2 to 6 weeks based on response and tolerability (Ref).

Alternative dosing (Ref):

ER capsule: 4 mg once daily; the dose may be lowered to 2 mg once daily based on individual response and tolerability.

IR tablet: 2 mg twice daily; the dose may be lowered to 1 mg twice daily based on individual response and tolerability.

Ureteral stent–related urinary symptoms, treatment

Ureteral stent–related urinary symptoms, treatment (off-label use):

Note: Other therapies (eg, selective alpha-1 blocker) may be preferred in individuals who may be sensitive to anticholinergic effects (eg, dry mouth, constipation) and in those with potential cognitive risks (Ref).

Oral: ER capsule: 4 mg once daily if needed following stent placement; may be given in combination with a selective alpha-1 blocker (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function:

CrCl >30 mL/minute: Oral: No dosage adjustment required (Ref).

CrCl 10 to ≤30 mL/minute:

Note: Use with caution as metabolites accumulate with chronic dosing; the clinical significance is not fully known but may include increased risk of QT/QTc prolongation (Ref).

IR tablet: Oral: 1 mg twice daily (Ref).

ER capsule: Oral: 2 mg once daily (Ref).

CrCl <10 mL/minute: Oral: Avoid use (Ref).

Augmented renal clearance (measured urinary CrCl ≥130 mL/minute/1.73m2):

Note: Augmented renal clearance (ARC) is a condition that occurs in certain critically ill patients without organ dysfunction and with normal SCr concentrations. Younger patients (<55 years of age) admitted post trauma or major surgery are at highest risk for ARC, as well as those with sepsis, burns, or hematologic malignancies. An 8- to 24-hour measured urinary CrCl is necessary to identify these patients (Ref).

Oral: No data; no dosage adjustment necessary (Ref).

Hemodialysis, intermittent (thrice weekly): Not expected to be significantly dialyzable based on high protein binding (>96%) (Ref):

Oral: Avoid use (Ref).

Peritoneal dialysis: Not expected to be significantly dialyzable based on high protein binding (>96%) (Ref):

Oral: Avoid use (Ref).

CRRT: Oral: Avoid use (Ref).

PIRRT (eg, sustained, low-efficiency diafiltration): Oral: Avoid use (Ref).

Dosing: Liver Impairment: Adult

Immediate release tablet: Significantly reduced hepatic function: 1 mg twice daily; use with caution

Extended release capsule:

Mild to moderate impairment (Child-Pugh class A or B): 2 mg once daily

Severe impairment (Child-Pugh class C): Use is not recommended; has not been studied.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Gastrointestinal: Xerostomia (23% to 35%)

1% to 10%:

Cardiovascular: Chest pain (2%)

Dermatologic: Xeroderma (1%)

Endocrine & metabolic: Weight gain (1%)

Gastrointestinal: Abdominal pain (4% to 5%), constipation (6% to 7%), diarrhea (4%), dyspepsia (3% to 4%)

Genitourinary: Dysuria (1% to 2%)

Infection: Infection (1%)

Nervous system: Anxiety (1%), dizziness (≤5%), drowsiness (3%), fatigue (2% to 4%), headache (6% to 7%), vertigo (≤5%)

Neuromuscular & skeletal: Arthralgia (2%)

Ophthalmic: Dry eye syndrome (3%), visual disturbance (1% to 2%)

Respiratory: Flu-like symptoms (3%), sinusitis (2%)

Postmarketing:

Cardiovascular: Palpitations, peripheral edema, tachycardia

Hypersensitivity: Anaphylaxis, angioedema

Nervous system: Confusion, disorientation, hallucination, memory impairment

Contraindications

Hypersensitivity to tolterodine or fesoterodine (both are metabolized to 5-hydroxymethyl tolterodine) or any component of the formulation; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema: Cases of angioedema have been reported; some cases have occurred after a single dose. Discontinue immediately if angioedema and associated difficulty breathing, airway obstruction, or hypotension develop.

• CNS effects: May cause drowsiness, dizziness, and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Dose reduction or discontinuation should be considered if CNS effects occur.

• QT prolongation: Has been associated with QTc prolongation at high (supratherapeutic) doses. The manufacturer recommends caution in patients with congenital prolonged QT or in patients receiving concurrent therapy with QTc-prolonging drugs (class Ia or III antiarrhythmics). However, the extent of QTc prolongation even at supratherapeutic dosages was less than 15 msec. Individuals who are CYP2D6 poor metabolizers or in the presence of inhibitors of CYP2D6 and CYP3A4 may be more likely to exhibit prolongation.

Disease-related concerns:

• Alzheimer disease: Preliminary data suggests that long-term use of anticholinergics may potentially adversely affect the clinical course of Alzheimer disease in patients receiving cholinesterase inhibitors (Lu 2003; Sink 2008). Additional monitoring for decreases in cognition, functional abilities and increased problematic behaviors should be considered in patients with dementia receiving dual therapy with an acetylcholinesterase inhibitor and a bladder anticholinergic, such as tolterodine.

• Bladder flow obstruction: Use with caution in patients with bladder flow obstruction (eg, benign prostatic hypertrophy); may increase the risk of urinary retention.

• GI obstructive disorders: Use with caution in patients with decreased GI motility or gastrointestinal obstructive disorders (ie, pyloric stenosis); may increase the risk of gastric retention.

• Glaucoma: Use with caution in patients with controlled (treated) narrow-angle glaucoma.

• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment is required.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment is required.

Concurrent drug therapy issues:

• CYP3A4 inhibitors: Dosage adjustment is recommended in patients receiving CYP3A4 inhibitors; a lower dose of tolterodine is recommended.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule Extended Release 24 Hour, Oral, as tartrate:

Detrol LA: 2 mg [DSC], 4 mg [DSC] [contains fd&c blue #2 (indigotine,indigo carmine)]

Generic: 2 mg, 4 mg

Tablet, Oral, as tartrate:

Detrol: 1 mg [DSC], 2 mg

Generic: 1 mg, 2 mg

Generic Equivalent Available: US

Yes

Pricing: US

Capsule ER 24 Hour Therapy Pack (Tolterodine Tartrate ER Oral)

2 mg (per each): $8.04 - $13.14

4 mg (per each): $8.04 - $13.14

Tablets (Detrol Oral)

2 mg (per each): $10.39

Tablets (Tolterodine Tartrate Oral)

1 mg (per each): $1.00 - $3.31

2 mg (per each): $1.00 - $3.40

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule Extended Release 24 Hour, Oral, as tartrate:

Detrol LA: 2 mg, 4 mg [contains fd&c blue #2 (indigotine,indigo carmine)]

Generic: 2 mg, 4 mg

Tablet, Oral, as tartrate:

Detrol: 1 mg, 2 mg

Generic: 1 mg, 2 mg

Administration: Pediatric

Oral: Administer without regard to food; do not break, crush, or chew extended-release capsules.

Administration: Adult

ER capsule: Swallow whole; do not crush, chew, or open.

Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. IR tablet formulation is available. If safety and efficacy can be effectively monitored, no change in formulation or administration is required after bariatric surgery.

Storage/Stability

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light.

Use

Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence (FDA approved in adults)

Medication Safety Issues
Sound-alike/look-alike issues:

Tolterodine may be confused with fesoterodine, tolcapone

Detrol may be confused with Ditropan

Older Adult: High-Risk Medication:

Beers Criteria: Tolterodine is identified in the Beers Criteria as a potentially inappropriate medication in patients 65 years and older due to its strong anticholinergic properties (Beers Criteria [AGS 2023]).

Metabolism/Transport Effects

Substrate of CYP2C19 (Minor), CYP2C9 (Minor), CYP2D6 (Major), CYP3A4 (Major with inhibitors), CYP3A4 (Minor with inducers); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program

Acetylcholinesterase Inhibitors: May decrease therapeutic effects of Agents with Clinically Relevant Anticholinergic Effects. Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Acetylcholinesterase Inhibitors. Risk C: Monitor

Aclidinium: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Acrivastine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Agents with Clinically Relevant Anticholinergic Effects: May increase anticholinergic effects of Tolterodine. Risk C: Monitor

Ajmaline: May increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor

Amantadine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Artemether and Lumefantrine: May increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor

Benperidol: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Benperidol. Risk C: Monitor

Benztropine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Benztropine. Risk C: Monitor

Biperiden: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Biperiden. Risk C: Monitor

Bornaprine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Bornaprine. Risk C: Monitor

Botulinum Toxin-Containing Products: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Bromperidol: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Bromperidol. Risk C: Monitor

Buclizine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Buclizine. Risk C: Monitor

Cannabinoid-Containing Products: Agents with Clinically Relevant Anticholinergic Effects may increase tachycardic effects of Cannabinoid-Containing Products. Risk C: Monitor

Chlorprothixene: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Chlorprothixene. Risk C: Monitor

Cimetropium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Cimetropium. Risk X: Avoid

Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor

CloZAPine: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider Therapy Modification

Cyclizine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

CYP2D6 Inhibitors (Strong): May increase serum concentration of Tolterodine. Risk C: Monitor

CYP3A4 Inhibitors (Moderate): May increase serum concentration of Tolterodine. Risk C: Monitor

CYP3A4 Inhibitors (Strong): May increase serum concentration of Tolterodine. Management: The maximum recommended dose of tolterodine is 2 mg per day (1 mg twice daily for immediate-release tablets or 2 mg daily for extended-release capsules) when used together with a strong CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Darifenacin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Darifenacin. Risk C: Monitor

Dicyclomine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Dicyclomine. Risk C: Monitor

Dimethindene (Systemic): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Dimethindene (Systemic). Risk C: Monitor

DroNABinol: Agents with Clinically Relevant Anticholinergic Effects may increase tachycardic effects of DroNABinol. Risk X: Avoid

Eluxadoline: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of Eluxadoline. Risk X: Avoid

Fesoterodine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Fesoterodine. Risk C: Monitor

FluPHENAZine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification

Gastrointestinal Agents (Prokinetic): Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Gastrointestinal Agents (Prokinetic). Risk C: Monitor

Gepotidacin: May decrease anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Glucagon: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor

Glycopyrrolate (Oral Inhalation): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Glycopyrrolate (Oral Inhalation). Risk X: Avoid

Glycopyrrolate (Systemic): Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Glycopyrrolate (Systemic). Risk C: Monitor

Glycopyrronium (Topical): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Grapefruit Juice: May increase serum concentration of Tolterodine. Risk C: Monitor

Ipratropium (Nasal): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Ipratropium (Oral Inhalation): May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Itopride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Itopride. Risk C: Monitor

Levosulpiride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Levosulpiride. Risk X: Avoid

Maprotiline: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Maprotiline. Risk C: Monitor

Mavorixafor: May increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk X: Avoid

Melperone: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Methotrimeprazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Methotrimeprazine. Risk C: Monitor

Methscopolamine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Methscopolamine. Risk C: Monitor

Mirabegron: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Mirabegron. Risk C: Monitor

Nitroglycerin: Agents with Clinically Relevant Anticholinergic Effects may decrease absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor

OLANZapine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of OLANZapine. Risk C: Monitor

Opioid Agonists: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor

Opipramol: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Oxatomide: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

OxyBUTYnin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of OxyBUTYnin. Risk C: Monitor

Peginterferon Alfa-2b: May decrease serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Peginterferon Alfa-2b may increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor

Perazine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Perphenazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Perphenazine. Risk C: Monitor

Potassium Chloride: Agents with Clinically Relevant Anticholinergic Effects may increase ulcerogenic effects of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid

Potassium Citrate: Agents with Clinically Relevant Anticholinergic Effects may increase ulcerogenic effects of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid

Pramlintide: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. These effects are specific to the GI tract. Risk X: Avoid

Promethazine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Promethazine. Risk C: Monitor

Propantheline: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Propantheline. Risk C: Monitor

Propiverine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

QuiNIDine: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor

Ramosetron: Agents with Clinically Relevant Anticholinergic Effects may increase constipating effects of Ramosetron. Risk C: Monitor

Revefenacin: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Revefenacin. Risk X: Avoid

Rivastigmine: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Rivastigmine. Rivastigmine may decrease therapeutic effects of Agents with Clinically Relevant Anticholinergic Effects. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider Therapy Modification

Scopolamine: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Scopolamine. Risk C: Monitor

Secretin: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider Therapy Modification

Sofpironium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Sofpironium. Risk X: Avoid

Thiazide and Thiazide-Like Diuretics: Agents with Clinically Relevant Anticholinergic Effects may increase serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor

Thiothixene: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Thiothixene. Risk C: Monitor

Tiapride: Agents with Clinically Relevant Anticholinergic Effects may decrease therapeutic effects of Tiapride. Risk C: Monitor

Tiotropium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Tiotropium. Risk X: Avoid

Topiramate: Agents with Clinically Relevant Anticholinergic Effects may increase adverse/toxic effects of Topiramate. Risk C: Monitor

Trimethobenzamide: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Trimethobenzamide. Risk C: Monitor

Trospium: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Trospium. Risk C: Monitor

Umeclidinium: May increase anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk X: Avoid

Warfarin: Tolterodine may increase anticoagulant effects of Warfarin. Risk C: Monitor

Zuclopenthixol: Agents with Clinically Relevant Anticholinergic Effects may increase anticholinergic effects of Zuclopenthixol. Risk C: Monitor

Food Interactions

Food increases bioavailability (~53% increase) of tolterodine tablets (dose adjustment not necessary); does not affect the pharmacokinetics of tolterodine extended release capsules. As a CYP3A4 inhibitor, grapefruit juice may increase the serum level and/or toxicity of tolterodine, but unlikely secondary to high oral bioavailability. Management: Monitor patients closely with concurrent grapefruit juice use.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Mechanism of Action

Tolterodine is a competitive antagonist of muscarinic receptors. In animal models, tolterodine demonstrates selectivity for urinary bladder receptors over salivary receptors. Urinary bladder contraction is mediated by muscarinic receptors. Tolterodine increases residual urine volume and decreases detrusor muscle pressure.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Immediate release tablet: Rapid; ≥77%

Distribution: IV: Vd: 113 ± 27 L

Protein binding: >96% (primarily to alpha1-acid glycoprotein)

Metabolism: Extensively hepatic, primarily via CYP2D6 to 5-hydroxymethyltolterodine (active) and 3A4 usually (minor pathway). In patients with a genetic deficiency of CYP2D6, metabolism via 3A4 predominates.

Bioavailability: Immediate release tablet: Increased 53% with food

Half-life elimination:

Immediate release tablet: Extensive metabolizers: ~2 hours; Poor metabolizers: ~10 hours

Extended release capsule: Extensive metabolizers: ~7 hours; Poor metabolizers: ~18 hours

Time to peak: Immediate release tablet: 1-2 hours; Extended release capsule: 2-6 hours

Excretion: Urine (77%); feces (17%); primarily as metabolites (<1% unchanged drug) of which the active 5-hydroxymethyl metabolite accounts for 5% to 14% (<1% in poor metabolizers); as unchanged drug (<1%; <2.5% in poor metabolizers)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function: In patients with CrCl 10 to 30 mL/min, immediate-release tolterodine and metabolite levels were 2- to 3-fold higher compared with healthy patients. ER tolterodine has not been studied in patients with CrCl less than 10 mL/min.

Hepatic function impairment: The elimination half-life of immediate-release tolterodine was longer and Cl was substantially lower in cirrhotic patients compared with healthy patients.

Older adult: Serum concentrations of immediate-release tolterodine and 5-HMT were 20% to 50% higher in elderly patients.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Detrusitol;
  • (AR) Argentina: Breminal | Coli Q | Detrusitol | Toltem | Urginol;
  • (AT) Austria: Detrusitol | Tolterodin accord | Tolterodin Actavis | Tolterodin easypharm | Tolterodin pfizer | Tolterodin ratiopharm;
  • (AU) Australia: Detrusitol | Tolterodine tartrate;
  • (BD) Bangladesh: Detrusin | Terodin | Tolorin | Tolter | Toltrex | Ucol;
  • (BE) Belgium: Detrusitol | Tolterodine teva;
  • (BG) Bulgaria: Detrusitol;
  • (BR) Brazil: Detrusitol;
  • (CH) Switzerland: Detrusitol;
  • (CL) Chile: Detrusitol | Eltoven | Urostop;
  • (CN) China: Bu mai ding | Detrusitol | Le zai | Ning tong | She ni ting | Si pei er | Tolterodine tartra | Tolterodine tartrate;
  • (CO) Colombia: Detrusitol | Toldy | Tolterodina;
  • (CZ) Czech Republic: Detrusitol | Uroflow;
  • (DE) Germany: Detrusitol | Tolterodin | Tolterodin 1A Pharma | Tolterodin accord | Tolterodin Actavis | Tolterodin Hexal | Tolterodin pfizer | Tolterodin puren | Tolterodin ratiopharm | Tolterodine aristo;
  • (DO) Dominican Republic: Detrusitol | Eltoven;
  • (EC) Ecuador: Detrusitol | Eltoven | Tolterodina;
  • (EE) Estonia: Detrusitol | Tolterodine accord | Uroflow;
  • (EG) Egypt: Conturine | Cystoridine | Detrusitol | Incont | Noctopex | Sedoter | Terodine | Tolterodine | Urgeleve | Uricontrol;
  • (ES) Spain: Detrusitol | Urotrol;
  • (FI) Finland: Detrusitol;
  • (FR) France: Detrusitol | Tolterodine accord;
  • (GB) United Kingdom: Detrusitol | Tolterodine | Tolterodine Kent;
  • (GR) Greece: Detrulon | Detrusitol;
  • (HK) Hong Kong: Accord tolterodine | Detrusitol;
  • (HU) Hungary: Detrusitol;
  • (ID) Indonesia: Detrusitol;
  • (IE) Ireland: Detrusitol | Tolterodine tartrate;
  • (IL) Israel: Detrusitol;
  • (IN) India: Concyst | Detrusitol | Roliten | Terol La | Tolter | Tolu | Torq;
  • (IT) Italy: Detrusitol;
  • (JO) Jordan: Detrusitol;
  • (KR) Korea, Republic of: Binex tolterodin er | Binex Tolterodine | Ckd tolterodine sr | Derutol sr | Deterodine sr | Detrodin sr | Detrusitol | Dirutol | Eurocarin sr | Loxirodine | Neocitol sr | Olodin sr | Sedatol | Sedatol sr | Telodin | Toladine sr | Tolersta | Toloin | Tolostar | Toltarodin | Toltedin | Toltedine | Tolten | Tolterin | Tolteros sr | Toltomin | Tt rodine sr | Uretol | Urisis | Urocarine | Urodin | Urofree | Uroq sr | Urositol | Urotin S | Urotrol | Uterodin | Uvidi;
  • (KW) Kuwait: Detrusitol;
  • (LB) Lebanon: Detrusitol;
  • (LT) Lithuania: Detrusitol | Uroflow;
  • (LU) Luxembourg: Detrusitol | Tolterodin ratiopharm;
  • (LV) Latvia: Detrusitol;
  • (MA) Morocco: Urodine;
  • (MX) Mexico: Alarod | Asertral | Blad | Detrusitol | Dinafar | Fanerik | Ficsatol | Hipolter | Jania | Micrepis | Quimural | Tefilinb | Tolterodina | Tolterodina ultra | Ucrinix | Urotrol;
  • (MY) Malaysia: Detrusitol;
  • (NL) Netherlands: Detrusitol | Tolterodine;
  • (NO) Norway: Detrusitol | Tolterodin aristo;
  • (NZ) New Zealand: Arrow Tolterodine | Detrusitol;
  • (PE) Peru: Detrusitol | Terodin;
  • (PH) Philippines: Detrusitol;
  • (PK) Pakistan: Detriflow | Detrusitol | Ezeecon | Tolcare | Toldin | Tolferid | Tolter | Uniterole;
  • (PL) Poland: Defur | Detrusitol | Tolterodine accord | Uroflow | Uroflow sr;
  • (PR) Puerto Rico: Detrol | Tolterodine tartrate;
  • (PT) Portugal: Detrusitol;
  • (PY) Paraguay: Eltoven | Tolterodina imedic | Tornade;
  • (QA) Qatar: Blerone XL | Detrusitol | Detrusitol XL;
  • (RO) Romania: Uroflow;
  • (RU) Russian Federation: Detrusitol | Detruzitol | Roliten | Uroflex | Urotol;
  • (SA) Saudi Arabia: Detrusitol;
  • (SE) Sweden: Detrusitol | Tolterodin ebb | Tolterodin Orifarm | Tolterodin sandoz | Tolterodin teva | Tolterodine accord;
  • (SG) Singapore: Detrusitol;
  • (SI) Slovenia: Detrusitol;
  • (SK) Slovakia: Detrusitol;
  • (TH) Thailand: Detrusitol;
  • (TR) Turkey: Detrusitol | Toldin | Toltex;
  • (TW) Taiwan: Detrusitol | Terodine | Torodine;
  • (UA) Ukraine: Detrusitol | Roliten | Urotol;
  • (UY) Uruguay: Fluserin | Tolterox | Toltin;
  • (VE) Venezuela, Bolivarian Republic of: Detrusitol | Tolterodina;
  • (ZA) South Africa: Detrusitol
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